ES2616789T3 - Inhibidores de tirosina cinasa de Bruton - Google Patents
Inhibidores de tirosina cinasa de Bruton Download PDFInfo
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- ES2616789T3 ES2616789T3 ES12166300.9T ES12166300T ES2616789T3 ES 2616789 T3 ES2616789 T3 ES 2616789T3 ES 12166300 T ES12166300 T ES 12166300T ES 2616789 T3 ES2616789 T3 ES 2616789T3
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- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims description 2
- UPHOPMSGKZNELG-UHFFFAOYSA-N 2-hydroxynaphthalene-1-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)=C(O)C=CC2=C1 UPHOPMSGKZNELG-UHFFFAOYSA-N 0.000 claims description 2
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- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 claims description 2
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Families Citing this family (525)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2379308C2 (ru) * | 2004-04-02 | 2010-01-20 | Оси Фармасьютикалз, Инк. | 6, 6-бициклические кольцевые замещенные гетеробициклические ингибиторы протеинкиназ |
EP1906950A4 (en) * | 2005-06-21 | 2008-09-24 | Infinity Discovery Inc | ANSAMYCIN FORMULATIONS AND METHODS OF USE |
AU2007254179B2 (en) * | 2006-05-18 | 2013-03-21 | Pharmacyclics Llc | Intracellular kinase inhibitors |
BRPI0714963A2 (pt) * | 2006-08-16 | 2013-07-30 | Novartis Ag | processo de fabricaÇço de dispersÕes sàlidas de compostos terapÊuticos altamente cristalinos |
PL2529621T3 (pl) | 2006-09-22 | 2017-06-30 | Pharmacyclics Llc | Inhibitory kinazy tyrozynowej brutona |
ES2403546T3 (es) * | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
JP5347202B2 (ja) | 2007-03-28 | 2013-11-20 | ファーマサイクリックス,インク. | ブルトンチロシンキナーゼインヒビター |
US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
CA2684211A1 (en) * | 2007-04-12 | 2008-10-23 | Infinity Discovery, Inc. | Hydroquinone ansamycin formulations |
US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
US7982036B2 (en) * | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
US20110046144A1 (en) * | 2008-01-18 | 2011-02-24 | Mulvihill Mark J | Imidazopyrazinol derivatives for the treatment of cancers |
WO2009143051A1 (en) * | 2008-05-19 | 2009-11-26 | Osi Pharmaceuticals, Inc. | Substituted imidazopyr-and imidazotri-azines |
US20090301928A1 (en) * | 2008-06-05 | 2009-12-10 | United Comb & Novelty Corporation | Packaging For Lipped Containers |
US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
MX2010014029A (es) | 2008-06-27 | 2011-01-21 | Avila Therapeutics Inc | Compuestos de heteroarilo y usos de los mismos. |
US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
JP5318952B2 (ja) | 2008-07-15 | 2013-10-16 | エフ.ホフマン−ラ ロシュ アーゲー | 新規なフェニル−イミダゾピリジン類及びピリダジン類 |
CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
AU2013245503B2 (en) * | 2008-07-16 | 2015-09-24 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
CN102405284B (zh) * | 2008-09-05 | 2016-01-20 | 新基阿维罗米克斯研究公司 | 设计不可逆抑制剂的算法 |
WO2010043633A1 (en) * | 2008-10-15 | 2010-04-22 | Palau Pharma, S. A. | 2h-pyrazolo [4,3-d]pyrimidin-5-amine derivatives as h4 histamine receptor antagonists for the treatment of allergic, immunological and inflammatory diseases |
US8778921B2 (en) | 2008-10-15 | 2014-07-15 | Infinity Pharmaceuticals, Inc. | Ansamycin hydroquinone compositions |
US9095592B2 (en) * | 2008-11-07 | 2015-08-04 | The Research Foundation For The State University Of New York | Bruton's tyrosine kinase as anti-cancer drug target |
US8426428B2 (en) * | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
BRPI1016245A2 (pt) | 2009-04-20 | 2015-09-01 | Osi Pharmaceuticals Llc | Preparação de c-pirazina-metilaminas. |
US8765754B2 (en) | 2009-04-29 | 2014-07-01 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
EP2427192A1 (en) * | 2009-05-07 | 2012-03-14 | OSI Pharmaceuticals, LLC | Use of osi-906 for treating adrenocortical carcinoma |
EP3461824B1 (en) | 2009-09-04 | 2021-08-25 | Biogen MA Inc. | Bruton's tyrosine kinase inhibitors |
AU2010292116A1 (en) * | 2009-09-11 | 2012-05-03 | Cylene Pharmaceuticals Inc. | Pharmaceutically useful heterocycle-substituted lactams |
CN105063001A (zh) * | 2009-09-16 | 2015-11-18 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
US7965498B2 (en) | 2009-09-30 | 2011-06-21 | Apple Inc. | Cover glass to housing interface system |
US7718662B1 (en) * | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
WO2011090738A2 (en) | 2009-12-29 | 2011-07-28 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
CN102812167A (zh) | 2009-12-30 | 2012-12-05 | 阿维拉制药公司 | 蛋白的配体-介导的共价修饰 |
CA2792273A1 (en) * | 2010-03-08 | 2011-09-15 | Ratiopharm Gmbh | Dabigatran etexilate-containing pharmaceutical composition |
WO2011133609A2 (en) * | 2010-04-19 | 2011-10-27 | The Translational Genomics Research Institute | Methods and kits to predict therapeutic outcome of btk inhibitors |
HUE030720T2 (en) * | 2010-05-31 | 2017-06-28 | Ono Pharmaceutical Co | Purinone derivative as btk kinase inhibitor |
AU2011261185A1 (en) | 2010-06-03 | 2013-01-10 | Pharmacyclics, Inc. | The use of inhibitors of Bruton's tyrosine kinase (Btk) |
US20120053189A1 (en) * | 2010-06-28 | 2012-03-01 | Pharmacyclics, Inc. | Btk inhibitors for the treatment of immune mediated conditions |
CA2804648C (en) * | 2010-07-09 | 2019-01-22 | The Walter And Eliza Hall Institute Of Medical Research | Protein kinase inhibitors and methods of treatment |
MX336875B (es) | 2010-08-10 | 2016-02-04 | Celgene Avilomics Res Inc | Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk). |
WO2012022265A1 (en) * | 2010-08-20 | 2012-02-23 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
JP5956999B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | ヘテロアリール化合物およびその使用 |
SG10201508958WA (en) | 2010-11-01 | 2015-11-27 | Celgene Avilomics Res Inc | Heterocyclic Compounds And Uses Thereof |
JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | 変異体選択的egfr阻害剤およびその使用 |
AU2012221828C1 (en) | 2011-02-23 | 2015-10-01 | Pfizer Inc. | Imidazo[5,1-f][1,2,4]triazines for treatment of neurological disorders |
JP5974084B2 (ja) * | 2011-05-17 | 2016-08-23 | プリンシピア バイオファーマ インコーポレイテッド | チロシンキナーゼ阻害剤 |
WO2012158810A1 (en) * | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
AU2012255759B2 (en) | 2011-05-17 | 2017-08-10 | Principia Biopharma, Inc. | Kinase inhibitors |
WO2012158795A1 (en) | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
WO2013003629A2 (en) * | 2011-06-28 | 2013-01-03 | Pharmacyclics, Inc. | Methods and compositions for inhibition of bone resorption |
EP2726634B1 (en) | 2011-07-01 | 2017-02-22 | Dana-Farber Cancer Institute, Inc. | Discovery of a somatic mutation in myd88 gene in lymphoplasmacytic lymphoma |
EP2729466B1 (en) | 2011-07-08 | 2015-08-19 | Novartis AG | Novel pyrrolo pyrimidine derivatives |
EP2731612A4 (en) * | 2011-07-13 | 2015-04-08 | Pharmacyclics Inc | BRUTON TYROSINE KINASE HEMMER |
HUE041987T2 (hu) * | 2011-07-19 | 2019-06-28 | Merck Sharp & Dohme | 4-Imidazopiridazin-1-il-benzamidok és 4-imidazotriazin-1-il-benzamidok mint BTK-gátlók |
EP2548877A1 (en) * | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
EP3812387A1 (en) | 2011-07-21 | 2021-04-28 | Sumitomo Dainippon Pharma Oncology, Inc. | Heterocyclic protein kinase inhibitors |
AU2012325804B2 (en) * | 2011-10-19 | 2017-09-07 | Pharmacyclics Llc | Use of inhibitors of Bruton's tyrosine kinase (Btk) |
WO2013063401A1 (en) | 2011-10-28 | 2013-05-02 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
GB2496135B (en) | 2011-11-01 | 2015-03-18 | Valirx Plc | Inhibitors of the interaction between a Src family kinase and an androgen receptor or estradiol receptor for treatment of endometriosis |
UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
KR20140096100A (ko) * | 2011-11-03 | 2014-08-04 | 에프. 호프만-라 로슈 아게 | 이환 피페라진 화합물 |
US9212381B2 (en) * | 2011-11-10 | 2015-12-15 | President And Fellows Of Harvard College | Methods and compositions for labeling polypeptides |
US9382239B2 (en) | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
KR20180034705A (ko) | 2011-11-29 | 2018-04-04 | 오노 야꾸힝 고교 가부시키가이샤 | 퓨리논 유도체 염산염 |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
CA2862831A1 (en) | 2012-01-09 | 2013-07-18 | X-Rx, Inc. | Tryptoline derivatives having kinase inhibitory activity and uses thereof |
EP2809673B1 (en) * | 2012-01-31 | 2016-11-02 | Nanjing Allgen Pharma Co. Ltd. | Spirocyclic molecules as bruton's tyrosine kinase inhibitors |
US8501724B1 (en) | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
TW201336847A (zh) * | 2012-02-07 | 2013-09-16 | Taiho Pharmaceutical Co Ltd | 喹啉基吡咯并嘧啶化合物或其鹽 |
EP2722332B1 (en) * | 2012-02-23 | 2016-04-20 | Taiho Pharmaceutical Co., Ltd. | Quinolylpyrrolopyrimidyl fused-ring compound or salt thereof |
CN103312670A (zh) | 2012-03-12 | 2013-09-18 | 西安西电捷通无线网络通信股份有限公司 | 一种认证方法及系统 |
BR112014022789B1 (pt) | 2012-03-15 | 2022-04-19 | Celgene Car Llc | Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo |
KR102090453B1 (ko) | 2012-03-15 | 2020-03-19 | 셀젠 카르 엘엘씨 | 상피 성장 인자 수용체 키나제 억제제의 염 |
US9365566B2 (en) | 2012-03-27 | 2016-06-14 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives |
CN104203242B (zh) | 2012-04-04 | 2017-03-15 | 杭州德润玉成生物科技有限公司 | 取代的喹啉类作为布鲁顿酪氨酸激酶抑制剂 |
WO2013154778A1 (en) | 2012-04-11 | 2013-10-17 | Dana-Farber Cancer Institute, Inc. | Host targeted inhibitors of dengue virus and other viruses |
WO2013155347A1 (en) | 2012-04-11 | 2013-10-17 | Izumi Raquel | Bruton's tyrosine kinase inhibitors for hematopoietic mobilization |
CN103374001B (zh) * | 2012-04-19 | 2015-10-28 | 山东轩竹医药科技有限公司 | 咪唑并三嗪类mTOR抑制剂 |
KR101972990B1 (ko) * | 2012-05-31 | 2019-04-26 | 파마사이언스 인크. | 단백질 키나제 저해제 |
CA3218491A1 (en) | 2012-06-04 | 2013-12-12 | Pharmacyclics Llc | Crystalline forms of a bruton's tyrosine kinase inhibitor |
AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
EP2861599B1 (en) * | 2012-06-18 | 2019-12-18 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment of cancer and autoimmune diseases |
US20150140085A1 (en) | 2012-06-29 | 2015-05-21 | Principia Biopharma Inc. | Formulations comprising ibrutinib |
KR20180088926A (ko) | 2012-07-24 | 2018-08-07 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이 |
EA201590296A1 (ru) * | 2012-07-30 | 2015-07-30 | Консерт Фармасьютикалс Инк. | Дейтерированный ибрутиниб |
WO2014022569A1 (en) * | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
GEP201706748B (en) * | 2012-08-10 | 2017-10-10 | Boehringer Ingelheim Int | Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors |
CN103121999A (zh) * | 2012-08-29 | 2013-05-29 | 苏州迪飞医药科技有限公司 | 一种酪氨酸激酶抑制剂pci-32765的合成方法 |
EP2890691B1 (en) | 2012-08-31 | 2018-04-25 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
CA2882367C (en) | 2012-09-10 | 2021-11-09 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
CH706997A1 (en) | 2012-09-20 | 2014-03-31 | Ferag Ag | Access control on operating modules of a control unit. |
EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
USRE48175E1 (en) * | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
SG11201503459SA (en) | 2012-11-02 | 2015-06-29 | Pharmacyclics Inc | Tec family kinase inhibitor adjuvant therapy |
AU2013340345B2 (en) * | 2012-11-02 | 2016-10-27 | Pfizer Inc. | Bruton's tyrosine kinase inhibitors |
JP2015537033A (ja) | 2012-11-15 | 2015-12-24 | ファーマサイクリックス,インク. | キナーゼ阻害剤としてのピロロピリミジン化合物 |
AR104762A1 (es) | 2012-11-16 | 2017-08-16 | Bristol Myers Squibb Co | Moduladores de dihidropirazol gpr40 |
CN103848810A (zh) * | 2012-11-30 | 2014-06-11 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
JP2016503803A (ja) * | 2012-12-21 | 2016-02-08 | テバ ファーマシューティカル インダストリーズ リミティド | 酢酸グラチラマーの経粘膜送達 |
WO2014100748A1 (en) | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
WO2014113942A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
TW201441234A (zh) * | 2013-01-23 | 2014-11-01 | Merck Sharp & Dohme | Btk抑制劑 |
WO2014113932A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
CA2900012A1 (en) | 2013-02-08 | 2014-08-14 | Celgene Avilomics Research, Inc. | Erk inhibitors and uses thereof |
US20140357636A1 (en) * | 2013-02-21 | 2014-12-04 | Wayne Rothbaum | Treatment of Skeletal-Related Disorders |
WO2014129596A1 (ja) | 2013-02-22 | 2014-08-28 | 大鵬薬品工業株式会社 | 三環性化合物の製造方法及び当該製造方法により得ることができる三環性化合物 |
JO3377B1 (ar) | 2013-03-11 | 2019-03-13 | Takeda Pharmaceuticals Co | مشتقات بيريدينيل وبيريدينيل مندمج |
WO2014165253A1 (en) * | 2013-03-12 | 2014-10-09 | Nbip, Llc | Compositions and methods for preventing infection of a wound and for advancing the healing process |
CN103142601A (zh) * | 2013-03-13 | 2013-06-12 | 杭州雷索药业有限公司 | Pci-32765在制备抗血管生成类药物中的应用 |
DK2970205T3 (da) | 2013-03-14 | 2019-07-29 | Tolero Pharmaceuticals Inc | JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf |
KR20160006668A (ko) * | 2013-03-14 | 2016-01-19 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나제 억제제와 cyp3a4 억제제의 배합물 |
JP6403751B2 (ja) | 2013-03-14 | 2018-10-10 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 5−チアゾールカルボキサミン誘導体及びbtk阻害剤としてのその使用 |
KR20210091832A (ko) | 2013-03-15 | 2021-07-22 | 셀젠 카르 엘엘씨 | Mk2 억제제 및 이의 용도 |
US9156847B2 (en) | 2013-03-15 | 2015-10-13 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a medicament |
EA201591685A1 (ru) * | 2013-03-15 | 2016-01-29 | Янссен Фармацевтика Нв | Способы и промежуточные соединения для получения лекарственного препарата |
JP6495886B2 (ja) | 2013-03-15 | 2019-04-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害剤としての複素環式芳香族化合物 |
UY35468A (es) | 2013-03-16 | 2014-10-31 | Novartis Ag | Tratamiento de cáncer utilizando un receptor quimérico de antígeno anti-cd19 |
JP2016519684A (ja) | 2013-04-08 | 2016-07-07 | デニス エム ブラウン | 準最適に投与された薬物療法の有効性を改善するための及び/又は副作用を低減するための方法および組成物 |
BR112015025711A8 (pt) * | 2013-04-08 | 2019-12-17 | Janssen Pharmaceutica Nv | uso de ibrutinibe e coposição farmacêutica compreendendo ibrutinibe e um agente anticâncer |
US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
AU2014256633B2 (en) | 2013-04-25 | 2017-02-02 | Beigene Switzerland Gmbh | Fused heterocyclic compounds as protein kinase inhibitors |
GB2513615A (en) | 2013-05-01 | 2014-11-05 | Cancer Rec Tech Ltd | Medical use |
GB201309085D0 (en) | 2013-05-20 | 2013-07-03 | Redx Pharma Ltd | Compounds |
EP2999702A4 (en) | 2013-05-21 | 2017-01-11 | Jiangsu Medolution Ltd. | Substituted pyrazolopyrimidines as kinases inhibitors |
US9637487B2 (en) | 2013-07-02 | 2017-05-02 | Pharmacyclics Llc | Purinone compounds as kinase inhibitors |
MX2015018038A (es) | 2013-07-03 | 2016-03-16 | Hoffmann La Roche | Compuestos de heteroaril-piridona y aza-piridona-amida. |
CN105764502A (zh) | 2013-07-26 | 2016-07-13 | 现代化制药公司 | 改善比生群及其类似物及衍生物的治疗益处的组合方法 |
TWI649081B (zh) | 2013-08-02 | 2019-02-01 | 製藥公司 | 治療固態腫瘤之方法 |
EP2832358A1 (en) | 2013-08-02 | 2015-02-04 | Bionsil S.r.l. | Pharmaceutical kit for use in the treatment of colon and colorectal cancer |
WO2015023703A1 (en) | 2013-08-12 | 2015-02-19 | Pharmacyclics, Inc. | Methods for the treatment of her2 amplified cancer |
US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
CA3080200A1 (en) | 2013-09-13 | 2015-03-19 | Beigene Switzerland Gmbh | Anti-pd1 antibodies and their use as therapeutics and diagnostics |
BR112016006978A2 (pt) * | 2013-09-30 | 2017-08-01 | Pharmacyclics Llc | inibidores de tirosina quinase de bruton |
RU2677884C2 (ru) | 2013-09-30 | 2019-01-22 | Гуанчжоу Иннокэа Фарма Тек Ко., Лтд. | Замещенные никотинимидные ингибиторы втк, их получение и применение в терапии раковых, воспалительных и аутоиммунных заболеваний |
WO2015054197A1 (en) * | 2013-10-10 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors, alone or in combination with btk inhibitors, for treating non-hodgkin's lymphoma |
WO2015057992A1 (en) | 2013-10-16 | 2015-04-23 | Izumi Raquel | Btk inhibitors for hematopoietic mobilization |
WO2015058140A1 (en) | 2013-10-18 | 2015-04-23 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
WO2015058084A1 (en) | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
CA2922044A1 (en) * | 2013-10-18 | 2015-05-14 | Medivation Technologies, Inc. | Pyrazolo-, imidazolo- and pyrrolo-pyridine or -pyrimidine derivatives as inhibitors o brutons kinase (btk) |
WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
KR102452866B1 (ko) * | 2013-10-25 | 2022-10-07 | 파마싸이클릭스 엘엘씨 | 이식편 대 숙주 질환의 치료 및 예방 방법 |
WO2015061752A1 (en) * | 2013-10-25 | 2015-04-30 | Pharmacyclics, Inc. | Treatment using bruton's tyrosine kinase inhibitors and immunotherapy |
US9636340B2 (en) | 2013-11-12 | 2017-05-02 | Ayyappan K. Rajasekaran | Kinase inhibitors |
WO2015071432A1 (en) | 2013-11-14 | 2015-05-21 | Sandoz Ag | Pharmaceutical compositions of ibrutinib |
US20150141438A1 (en) * | 2013-11-15 | 2015-05-21 | Pharmacyclics, Inc. | Methods for delaying or preventing the onset of type 1 diabetes |
CN103626774B (zh) | 2013-11-20 | 2015-11-04 | 苏州明锐医药科技有限公司 | 伊鲁替尼的制备方法 |
CA2833867A1 (en) | 2013-11-21 | 2015-05-21 | Pharmascience Inc. | Protein kinase inhibitors |
CN103694241A (zh) | 2013-11-27 | 2014-04-02 | 苏州晶云药物科技有限公司 | Pci-32765的新晶型a及其制备方法 |
US9512084B2 (en) | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
EA201691020A1 (ru) * | 2013-12-02 | 2017-01-30 | Фармасайкликс Элэлси | Способы лечения и предотвращения вызываемой аллогенными антителами хронической болезни "трансплантат против хозяина" |
AU2014358868A1 (en) | 2013-12-05 | 2016-06-09 | Acerta Pharma B.V. | Therapeutic combination of a PI3K inhibitor and a BTK inhibitor |
CA2929918C (en) | 2013-12-05 | 2018-01-23 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
CN106061973B (zh) | 2013-12-05 | 2019-07-09 | 辉瑞公司 | 吡咯并[2,3-d]嘧啶基、吡咯并[2,3-b]吡嗪基和吡咯并[2,3-d]吡啶基丙烯酰胺 |
US9908872B2 (en) * | 2013-12-13 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
US9856223B2 (en) | 2013-12-13 | 2018-01-02 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
WO2015095102A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Btk inhibitors |
US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
US9637486B2 (en) | 2013-12-20 | 2017-05-02 | Merck Sharp & Dohme Corp. | Btk inhibitors |
US10272083B2 (en) | 2014-01-21 | 2019-04-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor |
CN105949198A (zh) * | 2014-01-29 | 2016-09-21 | 苏州晶云药物科技有限公司 | 依鲁替尼的新晶型及其制备方法 |
JP6486954B2 (ja) | 2014-01-29 | 2019-03-20 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害剤としてのピラゾール化合物 |
MX2016009403A (es) * | 2014-02-03 | 2016-09-16 | Cadila Healthcare Ltd | Compuestos heterociclicos. |
BR112016018948B1 (pt) | 2014-02-21 | 2023-01-17 | Principia Biopharma Inc | Uso de composto ou sal farmaceuticamente aceitável, ácido sulfônico ou sal de ácido carboxílico de composto, forma amorfa de sal farmaceuticamente aceitável de composto, composição farmacêutica e respectivo uso |
AU2015222865B2 (en) | 2014-02-28 | 2019-06-20 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
CA2942528A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics Inc. | Phospholipase c gamma 2 and resistance associated mutations |
GB201404987D0 (en) * | 2014-03-20 | 2014-05-07 | Redx Pharma Ltd | Compounds |
JP6528779B2 (ja) | 2014-03-25 | 2019-06-12 | 小野薬品工業株式会社 | びまん性大細胞型b細胞リンパ腫の予防および/または治療剤 |
US9884869B2 (en) * | 2014-03-27 | 2018-02-06 | Perrigo Api Ltd. | Ibrutinib solid forms and production process therefor |
WO2015151006A1 (en) * | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
WO2015181633A2 (en) | 2014-04-11 | 2015-12-03 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
WO2015185998A2 (en) * | 2014-04-11 | 2015-12-10 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase |
CN105017256A (zh) | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
CN105085474B (zh) * | 2014-05-07 | 2018-05-18 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
CN105085529A (zh) * | 2014-05-15 | 2015-11-25 | 广东东阳光药业有限公司 | 依鲁替尼新晶型及其制备方法 |
CN104086551B (zh) * | 2014-06-06 | 2016-09-21 | 人福医药集团股份公司 | 化合物及其制备方法和用途 |
GB201410430D0 (en) * | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
US9949971B2 (en) | 2014-06-17 | 2018-04-24 | Acerta Pharma B.V. | Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor and/or a JAK-2 inhibitor |
CN104945404B (zh) * | 2014-06-25 | 2018-09-14 | 广东东阳光药业有限公司 | 一种n-丙烯羰基哌啶衍生物的制备方法 |
AR101106A1 (es) * | 2014-07-02 | 2016-11-23 | Pharmacyclics Llc | Inhibidores de tirosina quinasa de bruton |
TWI687438B (zh) | 2014-07-03 | 2020-03-11 | 英屬開曼群島商百濟神州生物科技有限公司 | 抗pd-l1抗體及其作為治療及診斷之用途 |
CN105294571B (zh) | 2014-07-03 | 2019-04-23 | 浙江九洲药业股份有限公司 | 一种依鲁替尼中间体及其制备方法和用途 |
ES2706745T3 (es) | 2014-07-07 | 2019-04-01 | Jiangsu Hengrui Medicine Co | Compuestos de aminopiridazinona como inhibidores de proteína cinasa |
WO2016008411A1 (en) * | 2014-07-18 | 2016-01-21 | Beigene, Ltd. | 5-amino-4-carbamoyl-pyrazole compounds as selective and irreversible t790m over wt-egfr kinase inhibitors and use thereof |
WO2016019237A2 (en) * | 2014-07-31 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
EP3174539A4 (en) | 2014-08-01 | 2017-12-13 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase |
CN106573002A (zh) | 2014-08-07 | 2017-04-19 | 药品循环有限责任公司 | 布鲁顿氏酪氨酸激酶抑制剂的新型制剂 |
WO2016020901A1 (en) | 2014-08-07 | 2016-02-11 | Acerta Pharma B.V. | Methods of treating cancers, immune and autoimmune diseases, and inflammatory diseases based on btk occupancy and btk resynthesis rate |
EP3177366A4 (en) | 2014-08-08 | 2018-04-04 | Pharmacyclics LLC | Bruton's tyrosine kinase inhibitor combinations and uses thereof |
CN105461720B (zh) * | 2014-08-08 | 2019-08-06 | 南京圣和药业股份有限公司 | 吗啉类酪氨酸激酶抑制剂 |
TW201618773A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | Btk抑制劑、pi3k抑制劑、jak-2抑制劑、及/或cdk4/6抑制劑的治療組合物 |
WO2016024227A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
DK3179991T3 (da) | 2014-08-11 | 2021-12-06 | Acerta Pharma Bv | Terapeutiske kombinationer af en btk-inhibitor og en bcl-2-inhibitor |
WO2016024228A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor, a pd-1 inhibitor and/or a pd-l1 inhibitor |
US11311512B2 (en) | 2014-08-12 | 2022-04-26 | Monash University | Lymph directing prodrugs |
WO2016025561A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Forms and compositions of an erk inhibitor |
CA2958139A1 (en) | 2014-08-14 | 2016-02-18 | Assia Chemical Industries Ltd. | Solid state forms of ibrutinib |
JP6507234B2 (ja) | 2014-10-02 | 2019-04-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトンチロシンキナーゼ(btk)によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物 |
WO2016065138A1 (en) | 2014-10-22 | 2016-04-28 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
US9688629B2 (en) | 2014-10-24 | 2017-06-27 | Bristol-Myers Squibb Company | Indole carboxamide compounds |
CN107108604B (zh) | 2014-10-27 | 2020-07-24 | 豪夫迈·罗氏有限公司 | 制备三环内酰胺化合物的方法 |
CA2965558A1 (en) * | 2014-10-30 | 2016-05-06 | Sandoz Ag | Synthesis of substituted 1h-pyrazolo[3,4-d]pyrimidines |
US10196397B2 (en) | 2014-11-19 | 2019-02-05 | Sun Pharmaceutical Industries Limited | Process for the preparation of ibrutinib |
WO2016079216A1 (en) | 2014-11-20 | 2016-05-26 | Sandoz Ag | Physical forms of ibrutinib, a bruton's kinase inhibitor |
CN104447761A (zh) * | 2014-11-27 | 2015-03-25 | 广东东阳光药业有限公司 | 一种吡唑衍生物的制备方法 |
WO2016088074A1 (en) * | 2014-12-03 | 2016-06-09 | Dr. Reddy’S Laboratories Limited | Process for the preparation of amorphous ibrutinib |
AR102871A1 (es) | 2014-12-03 | 2017-03-29 | Pharmacyclics Llc | Métodos de tratamiento de fibrosis |
WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
CN104478884A (zh) * | 2014-12-05 | 2015-04-01 | 广东东阳光药业有限公司 | 一种中间体的制备方法 |
TW201702218A (zh) | 2014-12-12 | 2017-01-16 | 美國杰克森實驗室 | 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法 |
PL3233103T3 (pl) | 2014-12-18 | 2021-04-19 | Principia Biopharma Inc. | Leczenie pęcherzycy |
CN118005631A (zh) | 2014-12-18 | 2024-05-10 | 豪夫迈·罗氏有限公司 | 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途 |
CA2972239A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
WO2016106624A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Tertiary alcohol imidazopyrazine btk inhibitors |
WO2016106629A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2016106628A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2016106652A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Biarylether imidazopyrazine btk inhibitors |
CN105820168B (zh) * | 2015-01-09 | 2018-12-04 | 上海医药工业研究院 | 一种依鲁替尼中间体的制备方法 |
MA41350A (fr) * | 2015-01-14 | 2017-11-21 | Janssen Pharmaceutica Nv | Synthèse d'un inhibiteur de la tyrosine kinase de bruton |
US10266535B2 (en) | 2015-01-21 | 2019-04-23 | Hefei Institutes Of Physical Science, Chinese Academy Of Sciences | Inhibitor of FLT3 kinase and use thereof |
WO2016123504A1 (en) * | 2015-01-30 | 2016-08-04 | Pharmacyclics Llc | Btk inhibitor combinations and multidrug-resistance |
CZ201584A3 (cs) | 2015-02-09 | 2016-08-17 | Zentiva, K.S. | Sůl Ibrutinib sulfátu |
US10214532B2 (en) | 2015-02-12 | 2019-02-26 | Shanghai Dude Medical Science and Technology Co., Ltd. | Process for preparing ibrutinib |
WO2016132383A1 (en) * | 2015-02-18 | 2016-08-25 | Mylan Laboratories Limited | Process for the preparation of ibrutinib |
ES2930585T3 (es) | 2015-02-27 | 2022-12-19 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of proton tyrosine kinase inhibitor |
WO2016141044A1 (en) | 2015-03-04 | 2016-09-09 | Arizona Board Of Regents On Behalf Of Arizona State University | Erbb4 inhibitors and methods of use thereof |
US9717745B2 (en) | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
MA41828A (fr) | 2015-03-27 | 2018-01-30 | Pharmacyclics Llc | Co-cristaux d'un inhibiteur de la tyrosine kinase de bruton |
MA41827A (fr) | 2015-03-27 | 2018-01-30 | Pharmacyclics Llc | Formes solvatées d'un inhibiteur de la tyrosine kinase de bruton |
EP3273966B1 (en) | 2015-03-27 | 2023-05-03 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2016161248A1 (en) * | 2015-04-02 | 2016-10-06 | Tolero Pharmaceuticals, Inc. | Targeting pim kinases in combination with btk inhibition |
KR102618114B1 (ko) * | 2015-04-02 | 2023-12-27 | 라티오팜 게엠베하 | 이브루티닙과 카복실산의 공결정체 |
CN106146511A (zh) * | 2015-04-03 | 2016-11-23 | 安润医药科技(苏州)有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
WO2016164404A1 (en) | 2015-04-06 | 2016-10-13 | Janssen Pharmaceutica Nv | Compositions containing ibrutinib |
CN105906621A (zh) * | 2015-04-06 | 2016-08-31 | 四川百利药业有限责任公司 | 用作fgfr抑制剂的乙醇类化合物 |
SG11201708191XA (en) | 2015-04-08 | 2017-11-29 | Novartis Ag | Cd20 therapies, cd22 therapies, and combination therapies with a cd19 chimeric antigen receptor (car) - expressing cell |
JP6750613B2 (ja) | 2015-04-09 | 2020-09-02 | 小野薬品工業株式会社 | プリノン誘導体の製造方法 |
CN106146512B (zh) * | 2015-04-09 | 2018-07-17 | 北京睿创康泰医药研究院有限公司 | 依鲁替尼的制备方法 |
US10485794B2 (en) | 2015-04-13 | 2019-11-26 | Daiichi Sankyo Company, Limited | Treatment method by combined use of MDM2 inhibitor and BTK inhibitor |
CN106146482B (zh) * | 2015-04-14 | 2020-06-23 | 宁波文达医药科技有限公司 | 布鲁顿酪氨酸激酶抑制剂 |
WO2016170545A1 (en) * | 2015-04-22 | 2016-10-27 | Msn Laboratories Private Limited | Process for the preparation of 1-[(3r)-3-[4-amino-3-(4-phenoxyphenvl)-1h- pvrazolo[3,4-d]pyriniidin-1-y1]-1-piperidinvl]-2-propen-1-one and its polymorphs thereof |
JP6847855B2 (ja) | 2015-04-30 | 2021-03-24 | バイエル ファーマ アクチエンゲゼルシャフト | Irak4の阻害剤とbtkの阻害剤の組み合わせ |
EP3195865A1 (de) | 2016-01-25 | 2017-07-26 | Bayer Pharma Aktiengesellschaft | Kombinationen von irak4 inhibitoren und btk inhibitoren |
RU2756010C2 (ru) | 2015-05-26 | 2021-09-24 | МорфоСис АГ | Комбинация антитела к CD19 и ингибитора тирозинкиназы брутона и их применение |
CA2987335A1 (en) | 2015-06-03 | 2016-12-08 | David Goldstein | Bruton tyrosine kinase inhibitors |
AU2016276963C1 (en) | 2015-06-12 | 2021-08-05 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
US9394312B1 (en) * | 2015-06-14 | 2016-07-19 | Mark Quang Nguyen | Ibrutinib prodrugs, pharmaceutical compositions thereof, and methods of use |
KR20180015160A (ko) | 2015-06-22 | 2018-02-12 | 오노 야꾸힝 고교 가부시키가이샤 | Brk 저해 화합물 |
EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
WO2016207172A1 (en) * | 2015-06-26 | 2016-12-29 | Sandoz Gmbh | Preparation of pure amorphous ibrutinib |
CZ2015442A3 (cs) * | 2015-06-26 | 2017-01-04 | Zentiva, K.S. | Ibrutinib hemisulfát |
WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
MA54252A (fr) | 2015-07-02 | 2022-04-27 | Hoffmann La Roche | Composés de benzoxazépine oxazolidinone et leurs procédés d'utilisation |
MX2018000179A (es) | 2015-07-02 | 2018-06-27 | Acerta Pharma Bv | Formas solidas y formulaciones de (s)-4-(8-amino-3-(1-(but-2-inoil )pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benz amida. |
WO2017001658A1 (en) | 2015-07-02 | 2017-01-05 | F. Hoffmann-La Roche Ag | Benzoxazepin oxazolidinone compounds and methods of use |
ITUB20152576A1 (it) * | 2015-07-29 | 2017-01-29 | Laboratorio Chimico Int S P A | Procedimento per la preparazione di ibrutinib e nuovo intermedio di sintesi. |
EP3337485B1 (en) | 2015-08-19 | 2021-03-17 | Sun Pharmaceutical Industries Ltd | Crystalline forms of ibrutinib |
WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
EP3344254A1 (en) | 2015-08-31 | 2018-07-11 | Pharmacyclics LLC | Btk inhibitor combinations for treating multiple myeloma |
JP6802263B2 (ja) | 2015-09-02 | 2020-12-16 | ニンバス ラクシュミ, インコーポレイテッド | Tyk2阻害剤およびその使用 |
CA2997106C (en) | 2015-09-08 | 2024-06-04 | Monash University | Lymph directing prodrugs |
EP4019515A1 (en) | 2015-09-09 | 2022-06-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2017044720A1 (en) | 2015-09-11 | 2017-03-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
CA2904270A1 (en) * | 2015-09-11 | 2017-03-11 | Pharmascience Inc. | Protein kinase inhibitors |
CN105753863B (zh) * | 2015-09-11 | 2018-07-31 | 东莞市真兴贝特医药技术有限公司 | 氧代二氢咪唑并吡啶类化合物及其应用 |
MA44909A (fr) | 2015-09-15 | 2018-07-25 | Acerta Pharma Bv | Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk |
US20190022092A1 (en) | 2015-09-15 | 2019-01-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist |
US10611766B2 (en) | 2015-09-16 | 2020-04-07 | Loxo Oncology Inc. | Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer |
TW201725044A (zh) | 2015-10-01 | 2017-07-16 | 基利科學股份有限公司 | 用於治療癌症之btk抑制劑及查核點抑制劑之組合 |
CN106608877B (zh) * | 2015-10-21 | 2018-11-13 | 新发药业有限公司 | 一种依鲁替尼中间体4-氨基-3-(4-苯氧基)苯基-1H-吡唑并[3,4-d]嘧啶的制备方法 |
CA3234750A1 (en) | 2015-10-23 | 2017-04-27 | Navitor Pharmaceuticals, Inc. | Modulators of sestrin-gator2 interaction and uses thereof |
TWI642671B (zh) | 2015-10-28 | 2018-12-01 | 台灣神隆股份有限公司 | 依魯替尼之製備方法及其中間體 |
PL3377484T3 (pl) * | 2015-11-17 | 2024-04-08 | Merck Patent Gmbh | Metody dla terapii stwardnienia rozsianego z użyciem związków pirymidynowych i pirydynowych z aktywnością inhibitorową dla btk |
CN105294696A (zh) * | 2015-11-19 | 2016-02-03 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
MA43377A (fr) | 2015-12-04 | 2021-05-19 | Hutchinson Fred Cancer Res | Méthodes et compositions liées à la toxicité associée à la thérapie cellulaire |
CN108367006B (zh) | 2015-12-04 | 2021-12-31 | 博尔托拉制药公司 | 用于治疗血液癌症的赛度替尼 |
JO3793B1 (ar) | 2015-12-10 | 2021-01-31 | Janssen Pharmaceutica Nv | مثبطات تيروزين كاينيز بروتون وأساليب استخدامها |
JO3794B1 (ar) | 2015-12-10 | 2021-01-31 | Janssen Pharmaceutica Nv | المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون |
US11370792B2 (en) | 2015-12-14 | 2022-06-28 | Raze Therapeutics, Inc. | Caffeine inhibitors of MTHFD2 and uses thereof |
MX2021003478A (es) | 2015-12-16 | 2022-07-25 | Loxo Oncology Inc | Compuestos utiles como inhibidores de cinasa. |
SI3390390T1 (sl) | 2015-12-16 | 2021-12-31 | Boehringer Ingelheim International Gmbh | Bipirazolilni derivati, uporabni za zdravljenje avtoimunskih bolezni |
WO2017122175A1 (en) | 2016-01-13 | 2017-07-20 | Acerta Pharma B.V. | Therapeutic combinations of an antifolate and a btk inhibitor |
WO2017123695A1 (en) | 2016-01-13 | 2017-07-20 | Boehringer Ingelheim International Gmbh | Isoquinolones as btk inhibitors |
US20190290650A1 (en) | 2016-01-19 | 2019-09-26 | Janssen Pharmaceutic Nv | Formulations/compositions comprising a btk inhibitor |
BR112018014590A2 (pt) | 2016-01-19 | 2018-12-11 | Janssen Pharmaceutica Nv | formulações/composições compreendendo um inibidor de btk |
US10793566B2 (en) | 2016-01-21 | 2020-10-06 | Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. | Bruton's tyrosine kinase inhibitors |
JP6950897B2 (ja) * | 2016-01-21 | 2021-10-13 | ジーボ・バイオポーラー・チャンシェン・ファーマシューティカル・カンパニー・リミテッドZibo Biopolar Changsheng Pharmaceutical Co. Ltd. | ブルトン型チロシンキナーゼ阻害剤 |
CN106995446B (zh) * | 2016-01-22 | 2021-07-02 | 山东新时代药业有限公司 | 布鲁顿酪氨酸激酶抑制剂制备方法 |
CN105732638B (zh) * | 2016-01-22 | 2018-01-30 | 成都倍特药业有限公司 | 一种具有螺环或桥环结构的布鲁顿酪氨酸激酶抑制剂及其制备方法 |
WO2017134684A2 (en) | 2016-02-01 | 2017-08-10 | Natco Pharma Limited | An improved process for the preparation of ibrutinib |
WO2017134685A2 (en) * | 2016-02-02 | 2017-08-10 | Sun Pharma Advanced Research Company Limited | Novel hydrazino compounds as btk inhibitors |
WO2017134588A1 (en) | 2016-02-04 | 2017-08-10 | Shilpa Medicare Limited | Process for the preparation of ibrutinib |
WO2017133630A1 (zh) * | 2016-02-05 | 2017-08-10 | 北京盛诺基医药科技有限公司 | 一种布鲁顿酪氨酸激酶抑制剂 |
GB2558514A (en) * | 2016-02-09 | 2018-07-18 | Azad Pharmaceutical Ingredients Ag | Process for the synthesis of stable amorphous ibrutinib |
WO2017143294A1 (en) | 2016-02-18 | 2017-08-24 | Privo Technologies, Inc. | Two-stage microparticle-based therapeutic delivery system and method |
CN105646498A (zh) * | 2016-03-01 | 2016-06-08 | 孙霖 | 依鲁替尼晶型f及制备方法 |
CN105646499A (zh) * | 2016-03-01 | 2016-06-08 | 孙霖 | 依鲁替尼晶型g及制备方法 |
ES2949357T3 (es) | 2016-03-09 | 2023-09-28 | Raze Therapeutics Inc | Inhibidores de 3-fosfoglicerato deshidrogenasa y usos de los mismos |
DK3426243T3 (da) | 2016-03-09 | 2021-07-19 | Raze Therapeutics Inc | 3-phosphoglyceratdehydrogenase-inhibitorer og anvendelser deraf |
CA3017567A1 (en) | 2016-03-11 | 2017-09-14 | Corvus Pharmaceuticals, Inc. | Compounds and methods for modulating bruton's tyrosine kinase |
WO2017163257A1 (en) * | 2016-03-21 | 2017-09-28 | Ind-Swift Laboratories Limited | Process for preparing pure lh-pyrazolo[3,4-d] pyrimidine derivative |
CN109071496B (zh) | 2016-03-31 | 2021-07-30 | 武田药品有限公司 | 异喹啉基三唑酮复合物 |
CZ2016196A3 (cs) | 2016-04-06 | 2017-10-18 | Zentiva, K.S. | Pevné formy Ibrutinibu |
JP2019510785A (ja) | 2016-04-08 | 2019-04-18 | エックス4 ファーマシューティカルズ, インコーポレイテッド | 癌を処置する方法 |
PL3442535T3 (pl) | 2016-04-15 | 2022-10-24 | Cancer Research Technology Limited | Związki heterocykliczne jako inhibitory kinazy ret |
CN115650985B (zh) | 2016-04-15 | 2024-08-02 | 癌症研究科技有限公司 | 作为ret激酶抑制剂的杂环化合物 |
WO2017184774A1 (en) | 2016-04-19 | 2017-10-26 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors, alone or in combination with btk inhibitors, for treating chronic lymphocytic leukemia |
EP3448390A1 (en) * | 2016-04-29 | 2019-03-06 | Dana-Farber Cancer Institute, Inc. | Hck as a therapeutic target in myd88 mutated diseases |
CZ2016276A3 (cs) | 2016-05-11 | 2017-11-22 | Zentiva, K.S. | Pevné formy volné báze ibrutinibu |
HUE066655T2 (hu) | 2016-05-20 | 2024-08-28 | Biohaven Therapeutics Ltd | Riluzol, riluzol elõgyógyszerek és riluzol analógok felhasználása immunterápiákkal rákok kezelésére |
CN105859728B (zh) * | 2016-05-26 | 2018-06-08 | 江苏中邦制药有限公司 | 一种依鲁替尼的制备方法 |
EA201892284A1 (ru) | 2016-05-27 | 2019-08-30 | Тг Терапьютикс, Инк. | Комбинация антитела против cd20, селективного ингибитора pi3-киназы-дельта и ингибитора btk для лечения b-клеточных пролиферативных расстройств |
WO2017216279A1 (en) | 2016-06-16 | 2017-12-21 | F. Hoffmann-La Roche Ag | Heteroaryl estrogen receptor modulators and uses thereof |
US20170362228A1 (en) | 2016-06-16 | 2017-12-21 | Genentech, Inc. | TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF |
ES2975263T3 (es) * | 2016-06-20 | 2024-07-04 | Novartis Ag | Formas cristalinas de un compuesto triazolopirimidínico |
CN116554168A (zh) | 2016-06-21 | 2023-08-08 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
CN109640988A (zh) | 2016-06-21 | 2019-04-16 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
JP6994767B2 (ja) | 2016-06-21 | 2022-01-14 | エックス4 ファーマシューティカルズ, インコーポレイテッド | Cxcr4阻害剤およびその使用 |
KR102515813B1 (ko) | 2016-06-29 | 2023-03-30 | 프린시피아 바이오파마, 인코퍼레이티드 | 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴의 변형 방출 제제 |
WO2018000250A1 (zh) * | 2016-06-29 | 2018-01-04 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
CN106117214A (zh) * | 2016-06-29 | 2016-11-16 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
SG11201811470PA (en) | 2016-06-30 | 2019-01-30 | Daewoong Pharmaceutical Co Ltd | Pyrazolopyrimidine derivatives as kinase inhibitor |
WO2018002958A1 (en) | 2016-06-30 | 2018-01-04 | Sun Pharma Advanced Research Company Limited | Novel hydrazide containing compounds as btk inhibitors |
WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
ES2965081T3 (es) | 2016-07-07 | 2024-04-11 | Daewoong Pharmaceutical Co Ltd | Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados |
CN107641123A (zh) * | 2016-07-20 | 2018-01-30 | 南京亿华药业有限公司 | 一种依鲁替尼及其关键中间体的制备新方法 |
SG11201900515PA (en) | 2016-07-21 | 2019-02-27 | Biogen Ma Inc | Succinate forms and compositions of bruton's tyrosine kinase inhibitors |
CA3033827A1 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl )-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide,preparation, and uses thereof |
WO2018033091A1 (zh) * | 2016-08-17 | 2018-02-22 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制酪氨酸激酶活性的稠合双环类化合物 |
TWI739887B (zh) | 2016-08-19 | 2021-09-21 | 英屬開曼群島商百濟神州有限公司 | 使用包含btk抑制劑的組合產品治療癌症 |
KR20190058550A (ko) | 2016-09-19 | 2019-05-29 | 메이 파마, 아이엔씨. | 병용 요법 |
CN109790121B (zh) * | 2016-10-06 | 2024-01-05 | 詹森药业有限公司 | 用于制备btk抑制剂的方法和中间体 |
TWI763722B (zh) | 2016-10-14 | 2022-05-11 | 美商林伯士拉克許米公司 | Tyk2抑制劑及其用途 |
JPWO2018074387A1 (ja) | 2016-10-17 | 2019-08-08 | 第一三共株式会社 | Mdm2阻害剤とdnaメチルトランスフェラーゼ阻害剤との併用治療法 |
JP7082120B2 (ja) | 2016-10-21 | 2022-06-07 | ニンバス ラクシュミ, インコーポレイテッド | Tyk2阻害剤およびその使用 |
CN110139669A (zh) | 2016-11-03 | 2019-08-16 | 朱诺治疗学股份有限公司 | T细胞疗法和btk抑制剂的组合疗法 |
US10414727B2 (en) | 2016-11-08 | 2019-09-17 | Navitor Pharmaceuticals, Inc. | Phenyl amino piperidine mTORC inhibitors and uses thereof |
WO2018090792A1 (zh) * | 2016-11-15 | 2018-05-24 | 杭州和正医药有限公司 | 一种选择性布鲁顿酪氨酸激酶抑制剂及其应用 |
CN108101905A (zh) * | 2016-11-24 | 2018-06-01 | 中国科学院上海药物研究所 | 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途 |
CA3043768A1 (en) | 2016-11-29 | 2018-06-07 | PureTech Health LLC | Exosomes for delivery of therapeutic agents |
US10183024B2 (en) | 2016-12-02 | 2019-01-22 | Apotex Inc. | Crystalline forms of ibrutinib |
US11590167B2 (en) | 2016-12-03 | 2023-02-28 | Juno Therapeutic, Inc. | Methods and compositions for use of therapeutic T cells in combination with kinase inhibitors |
US11091451B2 (en) | 2016-12-05 | 2021-08-17 | Raze Therapeutics, Inc. | SHMT inhibitors and uses thereof |
CN110291080B (zh) * | 2016-12-21 | 2022-07-08 | 安塞塔制药公司 | 布鲁顿酪氨酸激酶的咪唑并吡嗪抑制剂 |
JP2020502238A (ja) | 2016-12-23 | 2020-01-23 | バイスクルアールディー・リミテッド | 新規連結構造を有するペプチド誘導体 |
EP3565638B8 (en) | 2017-01-06 | 2024-04-10 | BicycleRD Limited | Bicycle conjugate for treating cancer |
EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) -PIPERIDINE-4-YL) -2- (4-PHENOXYPHENYL) -4,5,6,7-TETRAHYDROPYRAZOLO [1,5-A ] PYRIMIDINE-3-CARBOXAMIDE, MANUFACTURING AND USES THEREOF |
WO2018151849A1 (en) | 2017-02-17 | 2018-08-23 | Privo Technologies, Inc. | Particle-based multi-layer therapeutic delivery device and method |
JP2020508326A (ja) | 2017-02-24 | 2020-03-19 | ギリアド サイエンシズ, インコーポレイテッド | ブルトン型チロシンキナーゼの阻害剤 |
JP7014811B2 (ja) | 2017-02-24 | 2022-02-01 | ギリアド サイエンシズ, インコーポレイテッド | ブルトン型チロシンキナーゼの阻害剤 |
JP7160824B2 (ja) | 2017-03-08 | 2022-10-25 | ニンバス ラクシュミ, インコーポレイテッド | Tyk2阻害剤、使用およびその製造のための方法 |
CN108570036A (zh) * | 2017-03-09 | 2018-09-25 | 北京赛林泰医药技术有限公司 | 一种btk抑制剂的多晶型物及其制备方法 |
GB201703876D0 (en) | 2017-03-10 | 2017-04-26 | Berlin-Chemie Ag | Pharmaceutical combinations |
EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine derivatives |
WO2018170067A1 (en) * | 2017-03-14 | 2018-09-20 | Dana-Farber Cancer Institute, Inc. | Small molecule sensitization of bax activation for induction of cell death |
CN110494433B (zh) * | 2017-03-22 | 2023-03-17 | 廖细斌 | 布鲁顿酪氨酸激酶抑制剂 |
WO2018191146A1 (en) | 2017-04-10 | 2018-10-18 | Navitor Pharmaceuticals, Inc. | Heteroaryl rheb inhibitors and uses thereof |
GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
US10800787B2 (en) | 2017-04-20 | 2020-10-13 | Apotex Inc. | Process for the preparation of acalabrutinib |
CN107043366B (zh) * | 2017-04-25 | 2020-05-26 | 中国药科大学 | 4-氨基嘧啶类化合物、其制备方法及医药用途 |
AU2018258355B2 (en) | 2017-04-26 | 2024-05-30 | Navitor Pharmaceuticals, Inc. | Modulators of sestrin-gator2 interaction and uses thereof |
EP3615550A1 (en) | 2017-04-27 | 2020-03-04 | BicycleTx Limited | Bicyclic peptide ligands and uses thereof |
US10478403B1 (en) | 2017-05-03 | 2019-11-19 | Privo Technologies, Inc. | Intraoperative topically-applied non-implantable rapid release patch |
CN111225675B (zh) | 2017-06-02 | 2024-05-03 | 朱诺治疗学股份有限公司 | 使用过继细胞疗法治疗的制品和方法 |
CN111201438A (zh) | 2017-06-02 | 2020-05-26 | 朱诺治疗学股份有限公司 | 与和细胞疗法相关的毒性有关的制品和方法 |
CN109111446B (zh) * | 2017-06-22 | 2021-11-30 | 上海度德医药科技有限公司 | 一种具有药物活性的杂芳基化合物 |
EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | IMMUNOTHERAPY FOR LIVER CELL CARCINOMA |
EP3645549A1 (en) | 2017-06-26 | 2020-05-06 | BicycleRD Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
WO2019006427A1 (en) | 2017-06-29 | 2019-01-03 | Juno Therapeutics, Inc. | WALL MODEL FOR ASSESSING TOXICITIES ASSOCIATED WITH IMMUNOTHERAPIES |
WO2019013562A1 (ko) | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
KR102384924B1 (ko) | 2017-07-12 | 2022-04-08 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
CN111194317A (zh) | 2017-07-28 | 2020-05-22 | 林伯士拉克许米公司 | Tyk2抑制剂与其用途 |
WO2019025811A1 (en) | 2017-08-04 | 2019-02-07 | Bicycletx Limited | SPECIFIC BICYCLIC PEPTIDE LIGANDS OF CD137 |
US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
US20200283482A1 (en) | 2017-08-14 | 2020-09-10 | Bicyclerd Limited | Bicyclic peptide ligand prr-a conjugates and uses thereof |
WO2019034866A1 (en) | 2017-08-14 | 2019-02-21 | Bicyclerd Limited | BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF |
US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
AU2018324037A1 (en) | 2017-08-29 | 2020-04-16 | Monash University | Lymphatic system-directing lipid prodrugs |
WO2019046832A1 (en) | 2017-09-01 | 2019-03-07 | Juno Therapeutics, Inc. | GENE EXPRESSION AND EVALUATION OF RISK OF DEVELOPMENT OF TOXICITY FOLLOWING CELL THERAPY |
WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
EP3684365A4 (en) | 2017-09-22 | 2021-09-08 | Kymera Therapeutics, Inc. | PROTEIN DEGRADATION AGENTS AND USES OF SUCH |
EA037031B1 (ru) * | 2017-10-06 | 2021-01-28 | Асерта Фарма Б.В. | Имидазопиразиновые ингибиторы тирозинкиназы брутона |
KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
TW201922256A (zh) | 2017-10-27 | 2019-06-16 | 中國大陸商浙江導明醫藥科技有限公司 | 治療淋巴樣惡性疾病之方法 |
WO2019089848A1 (en) | 2017-11-01 | 2019-05-09 | Juno Therapeutics, Inc. | Methods associated with tumor burden for assessing response to a cell therapy |
WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
CZ2017787A3 (cs) | 2017-12-08 | 2019-06-19 | Zentiva, K.S. | Farmaceutické kompozice obsahující ibrutinib |
EP3727362A4 (en) | 2017-12-19 | 2021-10-06 | PureTech LYT, Inc. | MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES |
US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | IRAK joints and used in them |
CN108220261B (zh) * | 2017-12-29 | 2021-05-14 | 安徽联创生物医药股份有限公司 | 酮还原酶、核酸、重组表达载体、重组表达菌株及应用 |
US11485743B2 (en) | 2018-01-12 | 2022-11-01 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
US11512080B2 (en) | 2018-01-12 | 2022-11-29 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
CA3089537A1 (en) | 2018-01-20 | 2019-07-25 | Natco Pharma Limited | Pharmaceutical compositions comprising ibrutinib |
IL312674A (en) | 2018-01-29 | 2024-07-01 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
AU2019211485A1 (en) | 2018-01-29 | 2020-08-06 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
EP3759086A1 (en) | 2018-02-27 | 2021-01-06 | Artax Biopharma Inc. | Chromene derivatives as inhibitors of tcr-nck interaction |
MX2020010437A (es) | 2018-04-05 | 2021-01-29 | Sumitomo Pharma Oncology Inc | Inhibidores de axl cinasa y uso de los mismos. |
MX2020010556A (es) | 2018-04-13 | 2021-03-02 | Sumitomo Pharma Oncology Inc | Inhibidores de cinasa de insercion proviral en linfomas murinos (pim) para el tratamiento de neoplasias mieloproliferativas y fibrosis asociadas con cancer. |
JP7479293B2 (ja) | 2018-04-24 | 2024-05-08 | バーテックス ファーマシューティカルズ インコーポレイテッド | プテリジノン化合物およびその使用 |
HRP20220710T1 (hr) | 2018-04-24 | 2022-07-22 | Merck Patent Gmbh | Antiproliferacijski spojevi i njihova uporaba |
KR102106821B1 (ko) | 2018-04-27 | 2020-05-06 | 재단법인대구경북과학기술원 | 이브루티닙을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물 |
JP7331843B2 (ja) | 2018-04-27 | 2023-08-23 | 小野薬品工業株式会社 | Btk阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および/または治療剤 |
BR112020022185A2 (pt) | 2018-05-03 | 2021-02-02 | Juno Therapeutics Inc | terapia de combinação de uma terapia de células t do receptor de antígeno quimérico (car) e um inibidor de quinase |
TW202014412A (zh) | 2018-05-04 | 2020-04-16 | 美商普托拉製藥有限公司 | 賽度替尼(cerdulatinib)之固體型式 |
EP3575300A1 (en) | 2018-05-31 | 2019-12-04 | Apotex Inc. | Novel crystalline forms of ibrutinib |
IL259810A (en) | 2018-06-04 | 2018-07-31 | Yeda Res & Dev | Mitogen-activated protein kinase kinase 7 inhibitors |
RU2711106C2 (ru) * | 2018-06-06 | 2020-01-15 | Общество с ограниченной ответственностью "АКСЕЛЬФАРМ" | Кристаллическая μ-модификация 1-[(3R)-3-[4-амино-3-(4-фенокси-фенил)-1Н-пиразоло[3,4-d]пиримидин-1-ил]-1-пиперидил]-2-пропенил-1-она, способ её получения и фармацевтическая композиция на её основе |
CN112292117B (zh) | 2018-06-15 | 2024-06-07 | 詹森药业有限公司 | 包含依鲁替尼的配制品/组合物 |
FI3813946T3 (fi) | 2018-06-15 | 2024-06-25 | Janssen Pharmaceutica Nv | Rapamysiinianalogeja ja niiden käyttötapoja |
US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
US11040038B2 (en) | 2018-07-26 | 2021-06-22 | Sumitomo Dainippon Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same |
CN117281803A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
WO2020045941A1 (ko) | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
CA3111126A1 (en) | 2018-08-31 | 2020-03-05 | Stichting Katholieke Universiteit | Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof |
US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
CN110964016B (zh) * | 2018-09-29 | 2021-05-28 | 南京药捷安康生物科技有限公司 | 氨基降茨烷衍生物及其制备方法与应用 |
AU2019360941A1 (en) | 2018-10-15 | 2021-04-29 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
JP2022512779A (ja) | 2018-10-23 | 2022-02-07 | バイスクルテクス・リミテッド | 二環式ペプチドリガンドおよびその使用 |
MX2021004710A (es) | 2018-10-24 | 2021-06-04 | Navitor Pharm Inc | Compuestos polimorficos y usos de los mismos. |
CN111170986A (zh) | 2018-11-13 | 2020-05-19 | 北京睿熙生物科技有限公司 | 布鲁顿酪氨酸激酶的抑制剂 |
CN109293630A (zh) * | 2018-11-15 | 2019-02-01 | 山东大学 | 含取代吡唑类化合物及其制备方法与应用 |
CN109369654A (zh) * | 2018-11-20 | 2019-02-22 | 山东大学 | 1,3-二取代-4-氨基吡唑并嘧啶类化合物及其制备方法和应用 |
EP3886904A4 (en) | 2018-11-30 | 2022-07-13 | Kymera Therapeutics, Inc. | IRAQ-TYPE KINASE DEGRADING AGENTS AND THEIR USES |
WO2020113188A2 (en) | 2018-11-30 | 2020-06-04 | Juno Therapeutics, Inc. | Methods for dosing and treatment of b cell malignancies in adoptive cell therapy |
JP7530360B2 (ja) | 2018-11-30 | 2024-08-07 | 武田薬品工業株式会社 | Tyk2阻害剤およびその使用 |
AU2019387497A1 (en) | 2018-11-30 | 2021-06-24 | Juno Therapeutics, Inc. | Methods for treatment using adoptive cell therapy |
EP3670659A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Biomarkers, and uses in treatment of viral infections, inflammations, or cancer |
CN113453679A (zh) | 2018-12-20 | 2021-09-28 | C4医药公司 | 靶向蛋白降解 |
US10688050B1 (en) | 2018-12-21 | 2020-06-23 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
EP3669867A1 (en) | 2018-12-21 | 2020-06-24 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
JPWO2020130125A1 (ja) | 2018-12-21 | 2021-11-04 | 第一三共株式会社 | 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ |
WO2020144695A1 (en) | 2019-01-09 | 2020-07-16 | Yeda Research And Development Co. Ltd. | Modulators of pin1 activity and uses thereof |
CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药(上海)有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
EP3914357A4 (en) | 2019-01-23 | 2022-10-12 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND THEIR USES |
MX2021009371A (es) | 2019-02-12 | 2021-09-10 | Sumitomo Pharma Oncology Inc | Formulaciones que comprenden inhibidores de proteina cinasa heterociclicos. |
WO2020165600A1 (en) | 2019-02-14 | 2020-08-20 | Bicycletx Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
WO2020170270A1 (en) * | 2019-02-19 | 2020-08-27 | Msn Laboratories Private Limited, R&D Center | Novel crystalline polymorphs of 1-[(3r)-3-[4-amino-3-(4-phenoxyphenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one and process for preparation thereof |
CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
AU2020253990A1 (en) | 2019-04-02 | 2021-10-28 | Bicycletx Limited | Bicycle toxin conjugates and uses thereof |
TW202106676A (zh) | 2019-04-05 | 2021-02-16 | 美商凱麥拉醫療公司 | Stat降解劑及其用途 |
MX2021014245A (es) | 2019-05-21 | 2022-01-06 | Janssen Pharmaceutica Nv | Procedimientos y productos intermedios para preparar un inhibidor de btk. |
AU2020278162A1 (en) * | 2019-05-21 | 2021-11-18 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a BTK inhibitor |
US10937541B2 (en) * | 2019-05-28 | 2021-03-02 | PAIGE.AI, Inc. | Systems and methods for processing images to prepare slides for processed images for digital pathology |
US11458149B1 (en) | 2019-05-31 | 2022-10-04 | Ikena Oncology, Inc. | TEAD inhibitors and uses thereof |
TW202118770A (zh) | 2019-07-30 | 2021-05-16 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
WO2021038540A1 (en) | 2019-08-31 | 2021-03-04 | Sun Pharma Advanced Research Company Limited | Cycloalkylidene carboxylic acids and derivatives as btk inhibitors |
CA3150492A1 (en) | 2019-09-11 | 2021-03-18 | Donna L. Romero | USP30 INHIBITORS AND USES THEREOF |
CN114945366A (zh) | 2019-09-13 | 2022-08-26 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
MX2022005215A (es) | 2019-11-01 | 2022-06-08 | Navitor Pharm Inc | Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1). |
KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
KR20220128345A (ko) | 2019-12-05 | 2022-09-20 | 아나쿠리아 테라퓨틱스, 인코포레이티드 | 라파마이신 유사체 및 이의 용도 |
IL293393A (en) | 2019-12-06 | 2022-07-01 | Juno Therapeutics Inc | Cell therapy-related toxicity and response-related methods for the treatment of b-cell malignancies |
EP4076520A4 (en) | 2019-12-17 | 2024-03-27 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
MX2022007841A (es) | 2019-12-23 | 2022-07-19 | Kymera Therapeutics Inc | Degradadores del regulador dependiente de actina asociado a la matriz relacionado con el complejo switch/sacarosa no fermentable de la subfamilia a de la cromatina (smarca)y usos de los mismos. |
CN115348862A (zh) | 2020-01-20 | 2022-11-15 | 建新公司 | 用于复发型多发性硬化症(rms)的治疗性酪氨酸激酶抑制剂 |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2021159021A1 (en) | 2020-02-05 | 2021-08-12 | Puretech Lyt, Inc. | Lipid prodrugs of neurosteroids |
WO2021164697A1 (zh) * | 2020-02-18 | 2021-08-26 | 深圳市塔吉瑞生物医药有限公司 | 取代的酰胺衍生物及其组合物及用途 |
CN115151537B (zh) | 2020-02-26 | 2024-09-06 | 株式会社大熊制药 | 制备杂环胺衍生物的方法 |
AR121506A1 (es) | 2020-03-03 | 2022-06-08 | Pic Therapeutics Inc | Inhibidores del eif4e y sus usos |
JP2023518423A (ja) | 2020-03-19 | 2023-05-01 | カイメラ セラピューティクス, インコーポレイテッド | Mdm2分解剤およびそれらの使用 |
TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
CN114057724A (zh) * | 2020-07-29 | 2022-02-18 | 鲁南制药集团股份有限公司 | 一种btk抑制剂 |
WO2022038158A1 (en) | 2020-08-17 | 2022-02-24 | Bicycletx Limited | Bicycle conjugates specific for nectin-4 and uses thereof |
EP4203923A1 (en) | 2020-08-28 | 2023-07-05 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
WO2022047289A1 (en) * | 2020-08-28 | 2022-03-03 | Emory University | Methods of managing cocaine or other drug addictions |
WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
CA3200814A1 (en) | 2020-12-02 | 2022-06-09 | Alfredo C. Castro | Tead inhibitors and uses thereof |
JP2023553930A (ja) | 2020-12-10 | 2023-12-26 | ジェンザイム・コーポレーション | トレブルチニブの結晶形態、その製造方法、およびその使用 |
CN112574216B (zh) * | 2020-12-16 | 2022-03-08 | 天津济坤医药科技有限公司 | 一种化合物及其制备方法以及其在制备治疗抗癌药物中的应用 |
US20240092785A1 (en) | 2021-01-21 | 2024-03-21 | Synthon B.V. | Process for making ibrutinib |
JP2024505571A (ja) | 2021-02-02 | 2024-02-06 | リミナル・バイオサイエンシーズ・リミテッド | Gpr84アンタゴニストおよびその使用 |
CA3206499A1 (en) | 2021-02-02 | 2022-08-11 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
MX2023009178A (es) | 2021-02-15 | 2023-08-21 | Kymera Therapeutics Inc | Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos. |
EP4301756A1 (en) | 2021-03-05 | 2024-01-10 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
WO2022213062A1 (en) | 2021-03-29 | 2022-10-06 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
CA3215081A1 (en) | 2021-04-16 | 2022-10-20 | Alfredo C. Castro | Mek inhibitors and uses thereof |
MX2023013173A (es) | 2021-05-07 | 2023-11-30 | Kymera Therapeutics Inc | Degradadores de cinasa 2 dependiente de ciclina (cdk2) y sus usos. |
EP4346797A1 (en) * | 2021-06-01 | 2024-04-10 | Privo Technologies, Inc. | Enhanced two-stage microparticle-based localized therapeutic delivery system |
US11433072B1 (en) | 2021-06-10 | 2022-09-06 | Hikma Pharmaceuticals USA, Inc. | Oral dosage forms of ibrutinib |
WO2022260667A1 (en) | 2021-06-10 | 2022-12-15 | Hikma Pharmaceuticals Usa Inc. | Oral dosage forms of ibrutinib |
CN113583001A (zh) * | 2021-07-13 | 2021-11-02 | 江苏君若药业有限公司 | 依鲁替尼的制备 |
WO2023014817A1 (en) | 2021-08-03 | 2023-02-09 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating lymphomas with a cdk7 inhibitor in combination with a btk inhibitor |
CN115702898B (zh) * | 2021-08-04 | 2024-02-09 | 成都倍特药业股份有限公司 | 一种btk抑制剂固体制剂及其制备方法 |
US20230150997A1 (en) | 2021-08-25 | 2023-05-18 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
EP4392421A1 (en) | 2021-08-25 | 2024-07-03 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
CN113845521B (zh) * | 2021-08-31 | 2024-06-18 | 中原工学院 | 水相中光催化一锅法合成咪唑并含氮杂环肼类衍生物的方法 |
WO2023071973A1 (en) * | 2021-10-26 | 2023-05-04 | Shenzhen Targetrx, Inc. | Fused bicyclic compound for inhibiting activity of tyrosine kinase |
EP4444276A1 (en) | 2021-12-10 | 2024-10-16 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
WO2023114984A1 (en) | 2021-12-17 | 2023-06-22 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
US12091411B2 (en) | 2022-01-31 | 2024-09-17 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
CN114605418B (zh) * | 2022-03-15 | 2023-09-05 | 广东医科大学附属医院 | 一类具有抗肿瘤活性的依鲁替尼丙烯酰胺类衍生物及其合成方法与应用 |
WO2023211889A1 (en) | 2022-04-25 | 2023-11-02 | Ikena Oncology, Inc. | Polymorphic compounds and uses thereof |
WO2023220655A1 (en) | 2022-05-11 | 2023-11-16 | Celgene Corporation | Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy |
US11878958B2 (en) | 2022-05-25 | 2024-01-23 | Ikena Oncology, Inc. | MEK inhibitors and uses thereof |
US11884740B1 (en) | 2022-06-01 | 2024-01-30 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11807689B1 (en) | 2022-06-01 | 2023-11-07 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11814439B1 (en) | 2022-06-01 | 2023-11-14 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11965032B1 (en) | 2022-06-01 | 2024-04-23 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
WO2023242384A1 (en) | 2022-06-17 | 2023-12-21 | Krka, D.D., Novo Mesto | Crystalline form of ibrutinib |
TW202413364A (zh) * | 2022-06-22 | 2024-04-01 | 美商健臻公司 | 製備經修飾的btk抑制劑的方法 |
WO2024028365A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Substituted pyridone gpr84 antagonists and uses thereof |
TW202416950A (zh) | 2022-08-02 | 2024-05-01 | 英商利米那生物科技有限公司 | 雜芳基甲醯胺及相關gpr84拮抗劑及其用途 |
TW202415650A (zh) | 2022-08-02 | 2024-04-16 | 英商利米那生物科技有限公司 | 芳基-三唑基及相關gpr84拮抗劑及其用途 |
CN115417827B (zh) * | 2022-09-30 | 2023-05-26 | 中国药科大学 | 6-氨基-1,3,5-三嗪类化合物及其合成方法和应用 |
WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
WO2024112894A1 (en) | 2022-11-22 | 2024-05-30 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
Family Cites Families (160)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3993073A (en) | 1969-04-01 | 1976-11-23 | Alza Corporation | Novel drug delivery device |
US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
US3598122A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
US4069307A (en) | 1970-10-01 | 1978-01-17 | Alza Corporation | Drug-delivery device comprising certain polymeric materials for controlled release of drug |
US3731683A (en) | 1971-06-04 | 1973-05-08 | Alza Corp | Bandage for the controlled metering of topical drugs to the skin |
US3742951A (en) | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
US3996934A (en) | 1971-08-09 | 1976-12-14 | Alza Corporation | Medical bandage |
BE795384A (fr) | 1972-02-14 | 1973-08-13 | Ici Ltd | Pansements |
US3921636A (en) | 1973-01-15 | 1975-11-25 | Alza Corp | Novel drug delivery device |
US3993072A (en) | 1974-08-28 | 1976-11-23 | Alza Corporation | Microporous drug delivery device |
US4151273A (en) | 1974-10-31 | 1979-04-24 | The Regents Of The University Of California | Increasing the absorption rate of insoluble drugs |
US3972995A (en) | 1975-04-14 | 1976-08-03 | American Home Products Corporation | Dosage form |
US4077407A (en) | 1975-11-24 | 1978-03-07 | Alza Corporation | Osmotic devices having composite walls |
US4031894A (en) | 1975-12-08 | 1977-06-28 | Alza Corporation | Bandage for transdermally administering scopolamine to prevent nausea |
US4060084A (en) | 1976-09-07 | 1977-11-29 | Alza Corporation | Method and therapeutic system for providing chemotherapy transdermally |
US4201211A (en) | 1977-07-12 | 1980-05-06 | Alza Corporation | Therapeutic system for administering clonidine transdermally |
JPS5562012A (en) | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
US4230105A (en) | 1978-11-13 | 1980-10-28 | Merck & Co., Inc. | Transdermal delivery of drugs |
US4229447A (en) | 1979-06-04 | 1980-10-21 | American Home Products Corporation | Intraoral methods of using benzodiazepines |
CA1146866A (en) | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
US4291015A (en) | 1979-08-14 | 1981-09-22 | Key Pharmaceuticals, Inc. | Polymeric diffusion matrix containing a vasodilator |
US4327725A (en) | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
US5116817A (en) | 1982-12-10 | 1992-05-26 | Syntex (U.S.A.) Inc. | LHRH preparations for intranasal administration |
US4476116A (en) | 1982-12-10 | 1984-10-09 | Syntex (U.S.A.) Inc. | Polypeptides/chelating agent nasal compositions having enhanced peptide absorption |
US4596795A (en) | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
US4624848A (en) | 1984-05-10 | 1986-11-25 | Ciba-Geigy Corporation | Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use |
GB8518301D0 (en) | 1985-07-19 | 1985-08-29 | Fujisawa Pharmaceutical Co | Hydrodynamically explosive systems |
EP0230654B1 (en) | 1985-12-28 | 1992-03-18 | Sumitomo Pharmaceuticals Company, Limited | Sustained pulsewise release pharmaceutical preparation |
US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
US4968509A (en) | 1987-07-27 | 1990-11-06 | Mcneilab, Inc. | Oral sustained release acetaminophen formulation and process |
US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
JPH01167840A (ja) | 1987-12-24 | 1989-07-03 | Konica Corp | 新規な写真用シアンカプラー |
IL92966A (en) | 1989-01-12 | 1995-07-31 | Pfizer | Hydrogel-operated release devices |
US5739136A (en) | 1989-10-17 | 1998-04-14 | Ellinwood, Jr.; Everett H. | Intraoral dosing method of administering medicaments |
US5017381A (en) | 1990-05-02 | 1991-05-21 | Alza Corporation | Multi-unit pulsatile delivery system |
US5633009A (en) | 1990-11-28 | 1997-05-27 | Sano Corporation | Transdermal administration of azapirones |
EP0580860B2 (en) | 1991-04-16 | 2004-12-15 | Nippon Shinyaku Company, Limited | Method of manufacturing solid dispersion |
WO1993009785A1 (en) | 1991-11-22 | 1993-05-27 | Procter & Gamble Pharmaceuticals, Inc. | Risedronate delayed-release compositions |
US5229135A (en) | 1991-11-22 | 1993-07-20 | Prographarm Laboratories | Sustained release diltiazem formulation |
US5340591A (en) | 1992-01-24 | 1994-08-23 | Fujisawa Pharmaceutical Co., Ltd. | Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine |
US5461140A (en) | 1992-04-30 | 1995-10-24 | Pharmaceutical Delivery Systems | Bioerodible polymers for solid controlled release pharmaceutical compositions |
US5260068A (en) | 1992-05-04 | 1993-11-09 | Anda Sr Pharmaceuticals Inc. | Multiparticulate pulsatile drug delivery system |
US5281420A (en) | 1992-05-19 | 1994-01-25 | The Procter & Gamble Company | Solid dispersion compositions of tebufelone |
US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
AU4198793A (en) | 1992-07-24 | 1994-01-27 | Takeda Chemical Industries Ltd. | Microparticle preparation and production thereof |
US5700485A (en) | 1992-09-10 | 1997-12-23 | Children's Medical Center Corporation | Prolonged nerve blockade by the combination of local anesthetic and glucocorticoid |
ES2180548T3 (es) | 1992-10-16 | 2003-02-16 | Nippon Shinyaku Co Ltd | Metodo de obtencion de matrices de cera. |
US5260069A (en) | 1992-11-27 | 1993-11-09 | Anda Sr Pharmaceuticals Inc. | Pulsatile particles drug delivery system |
TW444018B (en) * | 1992-12-17 | 2001-07-01 | Pfizer | Pyrazolopyrimidines |
GB9226855D0 (en) | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
US5686105A (en) | 1993-10-19 | 1997-11-11 | The Procter & Gamble Company | Pharmaceutical dosage form with multiple enteric polymer coatings for colonic delivery |
US6326469B1 (en) | 1994-04-22 | 2001-12-04 | Sugen, Inc. | Megakaryocytic protein tyrosine kinases |
US5665378A (en) | 1994-09-30 | 1997-09-09 | Davis; Roosevelt | Transdermal therapeutic formulation |
US5530012A (en) | 1994-12-22 | 1996-06-25 | Bristol-Myers Squibb Co. | 3-alkoxybenzylpiperidine derivatives as melatonergic agents |
US5567441A (en) | 1995-03-24 | 1996-10-22 | Andrx Pharmaceuticals Inc. | Diltiazem controlled release formulation |
EP0827402A2 (en) | 1995-05-17 | 1998-03-11 | Cedars-Sinai Medical Center | Compositions containing fatty acids for improving digestion and absorption in the small intestine |
US5593997A (en) | 1995-05-23 | 1997-01-14 | Pfizer Inc. | 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors |
SE9502244D0 (sv) | 1995-06-20 | 1995-06-20 | Bioglan Ab | A composition and a process for the preparation thereof |
US5837284A (en) | 1995-12-04 | 1998-11-17 | Mehta; Atul M. | Delivery of multiple doses of medications |
US5858401A (en) | 1996-01-22 | 1999-01-12 | Sidmak Laboratories, Inc. | Pharmaceutical composition for cyclosporines |
CH690773A5 (de) | 1996-02-01 | 2001-01-15 | Novartis Ag | Pyrrolo(2,3-d)pyrimide und ihre Verwendung. |
US6929801B2 (en) | 1996-02-19 | 2005-08-16 | Acrux Dds Pty Ltd | Transdermal delivery of antiparkinson agents |
US6923983B2 (en) | 1996-02-19 | 2005-08-02 | Acrux Dds Pty Ltd | Transdermal delivery of hormones |
US6458373B1 (en) | 1997-01-07 | 2002-10-01 | Sonus Pharmaceuticals, Inc. | Emulsion vehicle for poorly soluble drugs |
HUP0001507A3 (en) | 1997-03-19 | 2002-01-28 | Abbott Gmbh & Co Kg | Pyrrolo [2,3-d] pyrimidine derivatives, process for their preparation, their use and pharmaceutical compositions containing them |
US5840329A (en) | 1997-05-15 | 1998-11-24 | Bioadvances Llc | Pulsatile drug delivery system |
US6391452B1 (en) | 1997-07-18 | 2002-05-21 | Bayer Corporation | Compositions for nasal drug delivery, methods of making same, and methods of removing residual solvent from pharmaceutical preparations |
US5869090A (en) | 1998-01-20 | 1999-02-09 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
JP2002512216A (ja) * | 1998-04-17 | 2002-04-23 | パーカー ヒューズ インスティテュート | Btkインヒビターならびにその同定方法および使用方法 |
US6303652B1 (en) * | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
US6335155B1 (en) | 1998-06-26 | 2002-01-01 | Sunesis Pharmaceuticals, Inc. | Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules |
US20050287596A9 (en) | 1998-06-26 | 2005-12-29 | Braisted Andrew C | Novel ligands and libraries of ligands |
US6998233B2 (en) | 1998-06-26 | 2006-02-14 | Sunesis Pharmaceuticals, Inc. | Methods for ligand discovery |
US6946144B1 (en) | 1998-07-08 | 2005-09-20 | Oryxe | Transdermal delivery system |
DE60039379D1 (de) | 1999-02-10 | 2008-08-21 | Pfizer Prod Inc | Pharmazeutische feste Dispersionen |
US6306897B1 (en) | 1999-03-19 | 2001-10-23 | Parker Hughes Institute | Calanolides for inhibiting BTK |
US6600744B1 (en) * | 1999-03-23 | 2003-07-29 | Alcatel Canada Inc. | Method and apparatus for packet classification in a data communication system |
US6395300B1 (en) | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
CZ2002936A3 (cs) | 1999-09-17 | 2002-10-16 | Abbott Gmbh & Co. Kg | Pyrazolopyrimidiny jako terapeutické prostředky |
JP5036112B2 (ja) | 1999-10-06 | 2012-09-26 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | チロシンキナーゼのインヒビターとして有益な複素環化合物 |
US6506769B2 (en) | 1999-10-06 | 2003-01-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
EP1235567A2 (en) | 1999-11-30 | 2002-09-04 | Parker Hughes Institute | Inhibitors of collagen-induced platelet aggregation |
EP1246829A1 (en) | 1999-12-17 | 2002-10-09 | Ariad Pharmaceuticals, Inc. | Novel heterocycles |
GB0005345D0 (en) | 2000-03-06 | 2000-04-26 | Mathilda & Terence Kennedy Ins | Methods of treating sepsis septic shock and inflammation |
AU2002236692A1 (en) | 2000-10-23 | 2002-05-21 | Bristol-Myers Squibb Company | Modulators of bruton's tyrosine kinase and bruton's tyrosine kinase, their identification and use |
JP2004514732A (ja) | 2000-12-06 | 2004-05-20 | ファルマシア・コーポレーション | 迅速に分散する医薬組成物 |
US6465014B1 (en) | 2001-03-21 | 2002-10-15 | Isp Investments Inc. | pH-dependent sustained release, drug-delivery composition |
MXPA03008560A (es) * | 2001-03-22 | 2004-06-30 | Abbot Gmbh & Co Kg | Pirazolopirimidinas como agentes terapeuticos. |
US8306897B2 (en) | 2001-05-04 | 2012-11-06 | Stockshield, Inc. | Method and system for insuring against investment loss |
ITMI20010995A1 (it) * | 2001-05-15 | 2002-11-15 | Getters Spa | Dispensatori di cesio e processo per il loro uso |
FI20011237A0 (fi) * | 2001-06-12 | 2001-06-12 | Nokia Corp | Tiedonsiirtomenetelmä ja -järjestely |
EP1463742A4 (en) | 2001-06-21 | 2006-05-10 | Ariad Pharma Inc | NEW PYRAZOLO AND PYRROLO PYRIMIDINES AND THEIR USES |
CA2810339A1 (en) | 2001-08-10 | 2003-02-20 | Novartis Ag | Use of c-src inhibitors alone or in combination with sti571 for the treatment of leukaemia |
WO2003016338A1 (en) | 2001-08-15 | 2003-02-27 | Parker Hughes Institute | Crystal structure of the btk kinase domain |
US6960563B2 (en) | 2001-08-31 | 2005-11-01 | Morton Grove Pharmaceuticals, Inc. | Spontaneous emulsions containing cyclosporine |
JP4391237B2 (ja) | 2001-11-21 | 2009-12-24 | サネシス ファーマシューティカルズ, インコーポレイテッド | リガンド発見のための方法 |
US6961787B2 (en) * | 2002-01-07 | 2005-11-01 | Intel Corporation | Method and apparatus for updating task files |
US20050084905A1 (en) | 2002-03-21 | 2005-04-21 | Prescott John C. | Identification of kinase inhibitors |
GB2388594A (en) | 2002-05-16 | 2003-11-19 | Bayer Ag | Imidazo-triazine PDE 4 inhibitors |
AU2003257094A1 (en) | 2002-08-08 | 2004-02-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted benzimidazole compounds |
GB0303910D0 (en) | 2003-02-20 | 2003-03-26 | Merck Sharp & Dohme | Therapeutic agents |
WO2005000197A2 (en) | 2003-04-11 | 2005-01-06 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
WO2004100868A2 (en) | 2003-04-23 | 2004-11-25 | Abbott Laboratories | Method of treating transplant rejection |
EP1473039A1 (en) | 2003-05-02 | 2004-11-03 | Centre National De La Recherche Scientifique (Cnrs) | Use of inhibitors and antisense oligonucleotides of BTK for the treatment of proliferative mastocytosis |
WO2005014599A1 (en) | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
WO2005005429A1 (en) | 2003-06-30 | 2005-01-20 | Cellular Genomics, Inc. | Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds |
US8131475B2 (en) | 2003-09-03 | 2012-03-06 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Methods for identifying, diagnosing, and predicting survival of lymphomas |
CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
US20070196395A1 (en) | 2003-12-12 | 2007-08-23 | Mackerell Alexander | Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain |
BRPI0418031A (pt) | 2003-12-22 | 2007-04-17 | Gilead Sciences Inc | inibidores de quinase fosfonato-substituìdos |
AU2005228845A1 (en) | 2004-01-26 | 2005-10-13 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
CA2553724A1 (en) | 2004-02-03 | 2005-08-18 | Abbott Laboratories | Aminobenzoxazoles as therapeutic agents |
ITMI20041314A1 (it) | 2004-06-30 | 2004-09-30 | Nuvera Fuel Cells Europ Srl | Dispositivo di raffreddamento per celle a combustibili a membrana |
WO2006036941A2 (en) * | 2004-09-27 | 2006-04-06 | Kosan Biosciences Incorporated | Specific kinase inhibitors |
US20060069123A1 (en) | 2004-09-28 | 2006-03-30 | Mingde Xia | Substituted dipiperidine CCR2 antagonists |
NZ555681A (en) * | 2004-11-10 | 2009-08-28 | Cgi Pharmaceuticals Inc | Imidazo[1, 2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
GB0425035D0 (en) * | 2004-11-12 | 2004-12-15 | Novartis Ag | Organic compounds |
CA2601628C (en) * | 2005-03-10 | 2014-05-13 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
EP1891066B1 (en) | 2005-05-13 | 2010-12-22 | Irm, Llc | Compounds and compositions as protein kinase inhibitors |
EP3088400A1 (en) | 2005-06-22 | 2016-11-02 | Plexxikon Inc. | Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors |
US20070065449A1 (en) | 2005-09-16 | 2007-03-22 | Claire Verschraegen | Method of treating cancer, especially soft tissue sarcoma utilizing gemcitabine in combination with docetaxel and anti-VEGF therapy (bevacizumab) |
WO2007058832A2 (en) | 2005-11-12 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Pyrrolo (2, 3-b) pyridine derivatives useful as tec kinase inhibitors |
CA2636696A1 (en) | 2006-01-13 | 2007-08-02 | Pharmacyclics, Inc. | Inhibitors of tyrosine kinases and uses thereof |
US20090317836A1 (en) | 2006-01-30 | 2009-12-24 | The Scripps Research Institute | Methods for Detection of Circulating Tumor Cells and Methods of Diagnosis of Cancer in Mammalian Subject |
PT2004654E (pt) * | 2006-04-04 | 2013-08-27 | Univ California | Derivados de pirazolopirimidina para utilização como antagonistas da quinase |
AU2007254179B2 (en) | 2006-05-18 | 2013-03-21 | Pharmacyclics Llc | Intracellular kinase inhibitors |
PL2529621T3 (pl) | 2006-09-22 | 2017-06-30 | Pharmacyclics Llc | Inhibitory kinazy tyrozynowej brutona |
ES2403546T3 (es) | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
NL2000640C2 (nl) | 2007-03-05 | 2008-09-08 | Stichting Wetsus Ct Of Excelle | Werkwijze en systeem voor het zuiveren van een vloeistof. |
US20120065201A1 (en) | 2007-03-28 | 2012-03-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
JP5347202B2 (ja) | 2007-03-28 | 2013-11-20 | ファーマサイクリックス,インク. | ブルトンチロシンキナーゼインヒビター |
US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
US20090010911A1 (en) | 2007-04-06 | 2009-01-08 | Iowa State University Research Foundation, Inc. | Methods and compositions for affecting cyclophilin a regulation of kinases in modulating cellular activities |
US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
SG185330A1 (en) | 2007-10-23 | 2012-11-29 | Hoffmann La Roche | Novel kinase inhibitors |
US8426441B2 (en) | 2007-12-14 | 2013-04-23 | Roche Palo Alto Llc | Inhibitors of bruton's tyrosine kinase |
US20150152115A1 (en) | 2007-12-27 | 2015-06-04 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
MX2010014029A (es) | 2008-06-27 | 2011-01-21 | Avila Therapeutics Inc | Compuestos de heteroarilo y usos de los mismos. |
CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
US8765754B2 (en) | 2009-04-29 | 2014-07-01 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
TWI380514B (en) * | 2009-07-09 | 2012-12-21 | Hon Hai Prec Ind Co Ltd | Electronic connector and electronic device using the same |
CN105063001A (zh) | 2009-09-16 | 2015-11-18 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
US20120071497A1 (en) | 2010-06-03 | 2012-03-22 | Pharmacyclics, Inc. | Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase |
AU2011261185A1 (en) | 2010-06-03 | 2013-01-10 | Pharmacyclics, Inc. | The use of inhibitors of Bruton's tyrosine kinase (Btk) |
RU2598852C2 (ru) | 2010-06-23 | 2016-09-27 | Ханми Сайенс Ко., Лтд. | Новые конденсированные пиримидиновые производные для ингибирования тирозинкиназной активности |
MX336875B (es) | 2010-08-10 | 2016-02-04 | Celgene Avilomics Res Inc | Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk). |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
US8501724B1 (en) | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
CA3218491A1 (en) | 2012-06-04 | 2013-12-12 | Pharmacyclics Llc | Crystalline forms of a bruton's tyrosine kinase inhibitor |
KR20180088926A (ko) | 2012-07-24 | 2018-08-07 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이 |
US20140377258A1 (en) | 2013-05-30 | 2014-12-25 | Infinity Pharmaceuticals, Inc. | Treatment Of Cancers Using PI3 Kinase Isoform Modulators |
TWI649081B (zh) | 2013-08-02 | 2019-02-01 | 製藥公司 | 治療固態腫瘤之方法 |
WO2015061752A1 (en) | 2013-10-25 | 2015-04-30 | Pharmacyclics, Inc. | Treatment using bruton's tyrosine kinase inhibitors and immunotherapy |
CN105949198A (zh) | 2014-01-29 | 2016-09-21 | 苏州晶云药物科技有限公司 | 依鲁替尼的新晶型及其制备方法 |
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